Thioethers: An Overview

2021 ◽  
Vol 22 ◽  
Author(s):  
M İhsan Han ◽  
Ş. Güniz Küçükgüzel
Keyword(s):  
Heterocyclic Compounds ◽  
Mortality Rates ◽  
Review Article ◽  
Cancer Development ◽  
Cancer Disease ◽  
Root Cause ◽  
New Class ◽  
Research Activities ◽  
Anti Cancer ◽  
Patent Literature

: Spreading rapidly in recent years, cancer has become the cause of one of the highest mortality rates after cardiovascular diseases. The reason for cancer development is still not clearly understood despite enormous research activities in this area. Scientists are now working on the biology of cancer, especially on the root cause of cancer development. The aim is to treat the cancer disease, and thus cure the patients. The continuing efforts on the development of novel molecules as potential anti-cancer agents are essential for this purpose. The main aim of this review was to present a survey on the medicinal chemistry of thioethers and to provide practical data on their cytotoxicities against various cancer cell lines. The research articles published between 2001-2020 were consulted in the preparation of this review article, though patent literature was not included here. The thioether-containing heterocyclic compounds may emerge as a new class of potent and effective anti-cancer agents soon.

Recent Developments in Anticancer Activity of Compounds Containing the Thioether Group

2020 ◽  
Vol 20 ◽  
Author(s):  
Muhammad İ. Han ◽  
Şükriye G. Küçükgüzel
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Research Field ◽  
Cancer Development ◽  
Anticancer Activities ◽  
Cancer Disease ◽  
New Class ◽  
Research Activities ◽  
Recent Developments ◽  
Patent Literature

Background: Spreading rapidly in recent years, cancer has become the cause of one of the highest mortality rates after cardiovascular diseases. With more attention being directed to cancer, anticancer research has become an important research field. In spite of enormous research activities in this area, the reason for cancer development is still not clearly understood. Scientists are now working on the biology of cancer, especially on the root of the cause for cancer development. The aim is to treat the cancer disease, and thus cure the patients. Continuing efforts on the development of novel molecules as potential anticancer agents is essential for this purpose. Objective: The main aim of this review was to present a survey on the medicinal chemistry of thioethers and to provide practical data on their cytotoxicities against various cancer cell lines. Methods: Research articles published between 2001-2019 were consulted in the preparation of this review article though patent literature was not included here. Results: Compounds containing thioether functionality were proven to have anticancer activities. Indeed, thioether functionality was found to be a must in some cases to show anticancer activity. Conclusion: Thioether containing molecules may emerge as new class of potent and effective anticancer agents in the near future.

scholarly journals Recent Advances in Chalcones: Synthesis, Transformation and Pharmacological Activities

2019 ◽  
pp. 1-16
Author(s):  
Oluwaseyi Bukky Ovonramwen ◽  
Bodunde Joseph Owolabi ◽  
Amowie Philip Oviawe
Keyword(s):  
Organic Synthesis ◽  
Heterocyclic Compound ◽  
Heterocyclic Compounds ◽  
Condensation Reaction ◽  
Review Article ◽  
Pharmacological Activities ◽  
Usual Approach ◽  
Recent Advances ◽  
Anti Cancer ◽  
Multifunctional Molecules

Chalcones are useful intermediates in the synthesis of heterocyclic compound and the unique reagents in organic synthesis. The usual approach to obtain chalcones is through Claisen-Schmidt condensation. Several novel heterocyclic chalcone analogs have emerged. Chalcones are multifunctional molecules that possess promising pharmacological activities. Chalcones are known for anti-cancer, antioxidant, anti-inflammatory, anti-microbial, anti-tubercular, antileishmanial, antimalarial, anthelmintic, osteogenic activities. This review article focuses on recent applications of Claisen-Schmidt condensation reaction employed in the synthesis of chalcone, its transformation to heterocyclic compounds and pharmacological activities.

N-heterocycles: Recent advances in biological applications

2021 ◽  
Vol 19 ◽  
Author(s):  
Monica Dinodia
Keyword(s):  
Structural Design ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Review Article ◽  
Biological Applications ◽  
Pharmacological Activities ◽  
Physiological Properties ◽  
Anti Cancer ◽  
Anti Hiv ◽  
Depth View

Abstract: Nitrogen based heterocycles display an impressive repertoire of biological activities, including antioxidant, antimicrobial, anti-tuberculosis, analgesic, anti-inflammatory, anti-viral, anti-HIV, anti-cancer, anti-helminthic, and other pharmacological activities. Numerous novel nitrogen-based heterocycles have been synthesized, which showed various physiological properties, and their application in medicinal chemistry is ever-growing. The present review will provide an in-depth view of N-heterocyclic compounds that showed biological activities in the last 5 years (2017-2021). This review article will be helpful for the structural design of effective and sustainable N-heterocyclic drugs against diseases with minimal side effects.

Amino-functional polyethers: versatile, stimuli-responsive polymers

2020 ◽  
Vol 11 (24) ◽  
pp. 3940-3950 ◽  
Author(s):  
Patrick Verkoyen ◽  
Holger Frey
Keyword(s):  
Ring Opening ◽  
Review Article ◽  
Stimuli Responsive ◽  
New Class ◽  
Stimuli Responsive Polymers ◽  
Responsive Polymers

Amino-functional polyethers have emerged as a new class of “smart”, i.e. pH- and thermoresponsive materials. This review article summarizes the synthesis and applications of these materials, obtained from ring-opening of suitable epoxide monomers.

Anodyne activities of New Tetrazole derivatives from Triazine

2020 ◽  
Vol 11 (3) ◽  
pp. 3377-3383
Author(s):  
Arulmozhi R ◽  
Abirami N ◽  
Helen P Kavitha ◽  
Arulmurugan S ◽  
Vinoth Kumar J
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Pharmaceutical Chemistry ◽  
Tail Flick ◽  
Structural Fragment ◽  
Hot Plate ◽  
Standard Drug ◽  
New Class ◽  
Novel Drugs ◽  
Tetrazole Derivatives

The creation of novel drugs containing a tetrazole ring as a structural fragment has contributed considerably to the outstanding achievements of the pharmaceutical chemistry in the last decade. Tetrazoles are the heterocyclic compounds having diverse biological activities such as analgesic, antiinflammation, antimicrobial, anticancer, antidiabetic, etc., and an impending source in biosciences. In this paper, the authors describe the synthesis of novel tetrazoles from N, N-( 6-Phenyl-1,3,5-triazine-2,4-diyl) dibenzamide (PTDDB) and 2-phenyl-4, 6-di(2H-tetrazole-2-yl)-1,3,5-triazine(5a-i) were prepared per the proposed scheme. A new class of tetrazole heterocycles were synthesised and characterised. I n vivo analysis was carried out on the analgesic property of synthesised tetrazole derivatives (5a, 5b, 5c). Characterisation studies such as IR, 1H NMR, 13C NMR, Mass and elemental analysis were performed for the synthesised tetrazole derivatives. Some of the tetrazole derivatives 5a, 5b, and 5c were tested for anodyne activity using morphine as the standard drug. The data reveals that all the three compounds 5a, 5b and 5c taken for the study show analgesic activity by hot plate method and tail flick methods. Among tested compounds, compound 5c is found to have potent analgesic (anodyne) activity. The results of the study indicate that the sample taken for the study show fairly good business using morphine as the standard drug.

Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

Biological role of AKT, and regulation of AKT signaling pathway by thymoquinone: perspectives in cancer therapeutics

2020 ◽  
Vol 20 ◽  
Author(s):  
Md. Junaid ◽  
Yeasmin Akter ◽  
Syeda Samira Afrose ◽  
Mousumi Tania ◽  
Md. Asaduzzaman Khan
Keyword(s):  
Clinical Trials ◽  
Signaling Pathways ◽  
Signaling Pathway ◽  
Inhibitory Effect ◽  
Akt Signaling ◽  
Review Article ◽  
Therapeutic Drug ◽  
Akt Signaling Pathway ◽  
Anti Cancer

Background: AKT/PKB is an important enzyme with numerous biological functions, and its overexpression is related to the carcinogenesis. AKT stimulates different signaling pathways that are downstream of activated tyrosine kinases and phosphatidylinositol 3-kinase, hence functions as an important target for anti-cancer drugs. Objective: In this review article, we have interpreted the role of AKT signaling pathways in cancer and natural inhibitory effect of Thymoquinone (TQ) in AKT and its possible mechanism. Method: We have collected the updated information and data on AKT, their role in cancer and inhibitory effect of TQ in AKT signaling pathway from google scholar, PubMed, Web of Science, Elsevier, Scopus and many more. Results: There are many drugs already developed, which can target AKT, but very few among them have passed clinical trials. TQ is a natural compound, mainly found in black cumin, which has been found to have potential anti-cancer activities. TQ targets numerous signaling pathways, including AKT, in different cancers. In fact, many studies revealed that AKT is one of the major targets of TQ. The preclinical success of TQ suggests its clinical studies on cancer. Conclusion: This review article summarizes the role of AKT in carcinogenesis, its potent inhibitors in clinical trials, and how TQ acts as an inhibitor of AKT and TQ’s future as a cancer therapeutic drug.

1,4-Dihydropyridine: A Dependable Heterocyclic Ring with the Promising and the Most Anticipable Therapeutic Effects

2019 ◽  
Vol 19 (15) ◽  
pp. 1219-1254 ◽  
Author(s):  
Abhinav Prasoon Mishra ◽  
Ankit Bajpai ◽  
Awani Kumar Rai
Keyword(s):  
Calcium Ion ◽  
Heterocyclic Compounds ◽  
Channel Blocker ◽  
Heterocyclic Ring ◽  
Therapeutic Effects ◽  
Voltage Gated ◽  
Therapeutic Benefits ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Synthetic Medicinal

: Nowadays, heterocyclic compounds act as a scaffold and are the backbone of medicinal chemistry. Among all of the heterocyclic scaffolds, 1,4-Dihydropyridine (1,4-DHP) is one of the most important heterocyclic rings that possess prominent therapeutic effects in a very versatile manner and plays an important role in synthetic, medicinal, and bioorganic chemistry. The main aim of the study is to review and encompass relevant studies related to 1,4-DHP and excellent therapeutic benefits of its derivatives. An extensive review of Pubmed-Medline, Embase and Lancet’s published articles was done to find all relevant studies on the activity of 1,4-DHP and its derivatives. 1,4-DHP is a potent Voltage-Gated Calcium Channel (VGCC) antagonist derivative which acts as an anti-hypertensive, anti- anginal, anti-tumor, anti-inflammatory, anti-tubercular, anti-cancer, anti-hyperplasia, anti-mutagenic, anti-dyslipidemic, and anti-ulcer agent. From the inferences of the study, it can be concluded that the basic nucleus, 1,4-DHP which is a voltage-gated calcium ion channel blocker, acts as a base for its derivatives that possess different important therapeutic effects. There is a need of further research of this basic nucleus as it is a multifunctional moiety, on which addition of different groups can yield a better drug for its other activities such as anti-convulsant, anti-oxidant, anti-mutagenic, and anti-microbial. This review would be significant for further researches in the development of several kinds of drugs by representing successful matrix for the medicinal agents.

Recent Advances in 1,3,5-Triazine Derivatives as Antibacterial Agents

2020 ◽  
Vol 17 (8) ◽  
pp. 991-1041
Author(s):  
Divya Utreja ◽  
Jagdish Kaur ◽  
Komalpreet Kaur ◽  
Palak Jain
Keyword(s):  
Antibacterial Activity ◽  
Heterocyclic Compounds ◽  
Antibacterial Agents ◽  
Rapid Development ◽  
Pharmacological Action ◽  
Biological Properties ◽  
Vast Array ◽  
Bacterial Diseases ◽  
New Class ◽  
Triazine Derivatives

Triazine, one of the nitrogen containing heterocyclic compounds has attracted the considerable interest of researchers due to the vast array of biological properties such as anti-viral, antitumor, anti-convulsant, analgesic, antioxidant, anti-depressant, herbicidal, insecticidal, fungicidal, antibacterial and anti-inflammatory activities offered by it. Various antibacterial agents have been synthesized by researchers to curb bacterial diseases but due to rapid development in drug resistance, tolerance and side effects, there had always been a need for the synthesis of a new class of antibacterial agents that would exhibit improved pharmacological action. Therefore, this review mainly focuses on the various methods for the synthesis of triazine derivatives and their antibacterial activity.

scholarly journals Combining Dextran Conjugates with Stimuli-Responsive and Folate-Targeting Activity: A New Class of Multifunctional Nanoparticles for Cancer Therapy

Nanomaterials ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 1108
Author(s):  
Manuela Curcio ◽  
Alessandro Paolì ◽  
Giuseppe Cirillo ◽  
Sebastiano Di Pietro ◽  
Martina Forestiero ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Drug Release ◽  
Metastatic Cancer ◽  
Stimuli Responsive ◽  
Cancer Disease ◽  
New Class ◽  
Self Assembling ◽  
Redox Responsive ◽  
Potential Applicability ◽  
Mean Size

Nanoparticles with active-targeting and stimuli-responsive behavior are a promising class of engineered materials able to recognize the site of cancer disease, targeting the drug release and limiting side effects in the healthy organs. In this work, new dual pH/redox-responsive nanoparticles with affinity for folate receptors were prepared by the combination of two amphiphilic dextran (DEX) derivatives. DEXFA conjugate was obtained by covalent coupling of the polysaccharide with folic acid (FA), whereas DEXssPEGCOOH derived from a reductive amination step of DEX was followed by condensation with polyethylene glycol 600. After self-assembling, nanoparticles with a mean size of 50 nm, able to be destabilized in acidic pH and reducing media, were obtained. Doxorubicin was loaded during the self-assembling process, and the release experiments showed the ability of the proposed system to modulate the drug release in response to different pH and redox conditions. Finally, the viability and uptake experiments on healthy (MCF-10A) and metastatic cancer (MDA-MB-231) cells proved the potential applicability of the proposed system as a new drug vector in cancer therapy.

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